Medicinal Radiochemistry
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Radiopharmacology is
radiochemistry Radiochemistry is the chemistry of radioactive materials, where radioactive isotopes of elements are used to study the properties and chemical reactions of non-radioactive isotopes (often within radiochemistry the absence of radioactivity leads t ...
applied to
medicine Medicine is the science and Praxis (process), practice of caring for patients, managing the Medical diagnosis, diagnosis, prognosis, Preventive medicine, prevention, therapy, treatment, Palliative care, palliation of their injury or disease, ...
and thus the
pharmacology Pharmacology is the science of drugs and medications, including a substance's origin, composition, pharmacokinetics, pharmacodynamics, therapeutic use, and toxicology. More specifically, it is the study of the interactions that occur betwee ...
of radiopharmaceuticals (
medicinal radiocompounds Radiopharmaceuticals, or medicinal radiocompounds, are a group of pharmaceutical drugs containing radioactive isotopes. Radiopharmaceuticals can be used as diagnostic and therapeutic agents. Radiopharmaceuticals emit radiation themselves, which ...
, that is,
pharmaceutical drug Medication (also called medicament, medicine, pharmaceutical drug, medicinal product, medicinal drug or simply drug) is a drug used to diagnose, cure, treat, or prevent disease. Drug therapy ( pharmacotherapy) is an important part of the ...
s that are
radioactive Radioactive decay (also known as nuclear decay, radioactivity, radioactive disintegration, or nuclear disintegration) is the process by which an unstable atomic nucleus loses energy by radiation. A material containing unstable nuclei is conside ...
). Radiopharmaceuticals are used in the field of
nuclear medicine Nuclear medicine (nuclear radiology, nucleology), is a medical specialty involving the application of radioactivity, radioactive substances in the diagnosis and treatment of disease. Nuclear imaging is, in a sense, ''radiology done inside out'', ...
as
radioactive tracer A radioactive tracer, radiotracer, or radioactive label is a synthetic derivative of a natural compound in which one or more atoms have been replaced by a radionuclide (a radioactive atom). By virtue of its radioactive decay, it can be used to ...
s in
medical imaging Medical imaging is the technique and process of imaging the interior of a body for clinical analysis and medical intervention, as well as visual representation of the function of some organs or tissues (physiology). Medical imaging seeks to revea ...
and in
therapy A therapy or medical treatment is the attempted remediation of a health problem, usually following a medical diagnosis. Both words, ''treatment'' and ''therapy'', are often abbreviated tx, Tx, or Tx. As a rule, each therapy has indications a ...
for many
disease A disease is a particular abnormal condition that adversely affects the structure or function (biology), function of all or part of an organism and is not immediately due to any external injury. Diseases are often known to be medical condi ...
s (for example,
brachytherapy Brachytherapy is a form of radiation therapy where a sealed radiation, radiation source is placed inside or next to the area requiring treatment. The word "brachytherapy" comes from the Ancient Greek, Greek word , meaning "short-distance" or "s ...
). Many radiopharmaceuticals use
technetium-99m Technetium-99m (99mTc) is a metastable nuclear isomer of technetium-99 (itself an isotope of technetium), symbolized as 99mTc, that is used in tens of millions of medical diagnostic procedures annually, making it the most commonly used Radiophar ...
(Tc-99m) which has many useful properties as a gamma-emitting tracer
nuclide Nuclides (or nucleides, from nucleus, also known as nuclear species) are a class of atoms characterized by their number of protons, ''Z'', their number of neutrons, ''N'', and their nuclear energy state. The word ''nuclide'' was coined by the A ...
. In the book ''Technetium'' a total of 31 different radiopharmaceuticals based on Tc-99m are listed for imaging and functional studies of the
brain The brain is an organ (biology), organ that serves as the center of the nervous system in all vertebrate and most invertebrate animals. It consists of nervous tissue and is typically located in the head (cephalization), usually near organs for ...
,
myocardium Cardiac muscle (also called heart muscle or myocardium) is one of three types of vertebrate muscle tissues, the others being skeletal muscle and smooth muscle. It is an involuntary, striated muscle that constitutes the main tissue of the wall o ...
,
thyroid The thyroid, or thyroid gland, is an endocrine gland in vertebrates. In humans, it is a butterfly-shaped gland located in the neck below the Adam's apple. It consists of two connected lobes. The lower two thirds of the lobes are connected by ...
,
lungs The lungs are the primary organs of the respiratory system in many animals, including humans. In mammals and most other tetrapods, two lungs are located near the backbone on either side of the heart. Their function in the respiratory syste ...
,
liver The liver is a major metabolic organ (anatomy), organ exclusively found in vertebrates, which performs many essential biological Function (biology), functions such as detoxification of the organism, and the Protein biosynthesis, synthesis of var ...
,
gallbladder In vertebrates, the gallbladder, also known as the cholecyst, is a small hollow Organ (anatomy), organ where bile is stored and concentrated before it is released into the small intestine. In humans, the pear-shaped gallbladder lies beneath t ...
,
kidneys In humans, the kidneys are two reddish-brown bean-shaped blood-filtering organs that are a multilobar, multipapillary form of mammalian kidneys, usually without signs of external lobulation. They are located on the left and right in the retro ...
,
skeleton A skeleton is the structural frame that supports the body of most animals. There are several types of skeletons, including the exoskeleton, which is a rigid outer shell that holds up an organism's shape; the endoskeleton, a rigid internal fra ...
,
blood Blood is a body fluid in the circulatory system of humans and other vertebrates that delivers necessary substances such as nutrients and oxygen to the cells, and transports metabolic waste products away from those same cells. Blood is com ...
and
tumor A neoplasm () is a type of abnormal and excessive growth of tissue. The process that occurs to form or produce a neoplasm is called neoplasia. The growth of a neoplasm is uncoordinated with that of the normal surrounding tissue, and persists ...
s. The term ''radioisotope'', which in its general
sense A sense is a biological system used by an organism for sensation, the process of gathering information about the surroundings through the detection of Stimulus (physiology), stimuli. Although, in some cultures, five human senses were traditio ...
refers to any radioactive
isotope Isotopes are distinct nuclear species (or ''nuclides'') of the same chemical element. They have the same atomic number (number of protons in their Atomic nucleus, nuclei) and position in the periodic table (and hence belong to the same chemica ...
(
radionuclide A radionuclide (radioactive nuclide, radioisotope or radioactive isotope) is a nuclide that has excess numbers of either neutrons or protons, giving it excess nuclear energy, and making it unstable. This excess energy can be used in one of three ...
), has historically been used to refer to all radiopharmaceuticals, and this usage remains common. Technically, however, many radiopharmaceuticals incorporate a
radioactive tracer A radioactive tracer, radiotracer, or radioactive label is a synthetic derivative of a natural compound in which one or more atoms have been replaced by a radionuclide (a radioactive atom). By virtue of its radioactive decay, it can be used to ...
atom into a larger pharmaceutically-active molecule, which is localized in the body, after which the radionuclide tracer atom allows it to be easily detected with a
gamma camera A gamma camera (γ-camera), also called a scintillation camera or Anger camera, is a device used to image gamma radiation emitting radioisotopes, a technique known as scintigraphy. The applications of scintigraphy include early drug development ...
or similar gamma imaging device. An example is fludeoxyglucose in which
fluorine-18 Fluorine-18 (18F, also called radiofluorine) is a fluorine radioisotope which is an important source of positrons. It has a mass of 18.0009380(6) u and its half-life is 109.771(20) minutes. It decays by positron emission 96.7% of the time and el ...
is incorporated into deoxyglucose. Some radioisotopes (for example gallium-67,
gallium-68 Natural gallium (31Ga) consists of a mixture of two stable Isotope, isotopes: gallium-69 and gallium-71. Twenty-nine radioisotopes are known, all synthetic, with atomic masses ranging from 60 to 89; along with three nuclear isomer, nuclear isomer ...
, and
radioiodine There are 40 known isotopes of iodine (53I) from 108I to 147I; all undergo radioactive decay except 127I, which is stable. Iodine is thus a monoisotopic element. Its longest-lived radioactive isotope, 129I, has a half-life of 16.14 million ye ...
) are used directly as soluble ionic salts, without further modification. This use relies on the chemical and biological properties of the radioisotope itself, to localize it within the body.


History

See
nuclear medicine Nuclear medicine (nuclear radiology, nucleology), is a medical specialty involving the application of radioactivity, radioactive substances in the diagnosis and treatment of disease. Nuclear imaging is, in a sense, ''radiology done inside out'', ...
.


Production

Production of a radiopharmaceutical involves two processes: * The production of the
radionuclide A radionuclide (radioactive nuclide, radioisotope or radioactive isotope) is a nuclide that has excess numbers of either neutrons or protons, giving it excess nuclear energy, and making it unstable. This excess energy can be used in one of three ...
on which the pharmaceutical is based. * The preparation and packaging of the complete radiopharmaceutical. Radionuclides used in radiopharmaceuticals are mostly radioactive
isotopes Isotopes are distinct nuclear species (or ''nuclides'') of the same chemical element. They have the same atomic number (number of protons in their nuclei) and position in the periodic table (and hence belong to the same chemical element), but ...
of elements with atomic numbers less than that of
bismuth Bismuth is a chemical element; it has symbol Bi and atomic number 83. It is a post-transition metal and one of the pnictogens, with chemical properties resembling its lighter group 15 siblings arsenic and antimony. Elemental bismuth occurs nat ...
, that is, they are radioactive isotopes of elements that also have one or more stable isotopes. These may be roughly divided into two classes: * Those with more neutrons in the nucleus than those required for stability are known as proton-deficient, and tend to be most easily produced in a
nuclear reactor A nuclear reactor is a device used to initiate and control a Nuclear fission, fission nuclear chain reaction. They are used for Nuclear power, commercial electricity, nuclear marine propulsion, marine propulsion, Weapons-grade plutonium, weapons ...
. The majority of radiopharmaceuticals are based on proton deficient isotopes, with
technetium-99m Technetium-99m (99mTc) is a metastable nuclear isomer of technetium-99 (itself an isotope of technetium), symbolized as 99mTc, that is used in tens of millions of medical diagnostic procedures annually, making it the most commonly used Radiophar ...
being the most commonly used medical isotope, and therefore nuclear reactors are the prime source of medical radioisotopes. * Those with fewer neutrons in the nucleus than those required for stability are known as neutron-deficient, and tend to be most easily produced using a proton accelerator such as a medical
cyclotron A cyclotron is a type of particle accelerator invented by Ernest Lawrence in 1929–1930 at the University of California, Berkeley, and patented in 1932. Lawrence, Ernest O. ''Method and apparatus for the acceleration of ions'', filed: Januar ...
.


Practical use

Because radiopharmeuticals require special licenses and handling techniques, they are often kept in local centers for medical radioisotope storage, often known as radiopharmacies. A radiopharmacist may dispense them from there, to local centers where they are handled at the practical medicine facility.


Drug nomenclature for radiopharmaceuticals

As with other pharmaceutical drugs, there is
standardization Standardization (American English) or standardisation (British English) is the process of implementing and developing technical standards based on the consensus of different parties that include firms, users, interest groups, standards organiza ...
of the
drug nomenclature Drug nomenclature is the systematic naming of drugs, especially pharmaceutical drugs. In the majority of circumstances, drugs have 3 types of names: chemical names, the most important of which is the IUPAC name; generic or nonproprietary names, ...
for radiopharmaceuticals, although various standards coexist. The International Nonproprietary Name (INN) gives the base drug name, followed by the radioisotope (as mass number, no space, element symbol) in parentheses with no superscript, followed by the ligand (if any). It is common to see square brackets and superscript superimposed onto the INN name, because
chemical nomenclature Chemical nomenclature is a set of rules to generate systematic name#In chemistry, systematic names for chemical compounds. The nomenclature used most frequently worldwide is the one created and developed by the International Union of Pure and Appli ...
(such as IUPAC nomenclature) uses those. The
United States Pharmacopeia The ''United States Pharmacopeia'' (''USP'') is a pharmacopeia (compendium of drug information) for the United States published annually by the over 200-year old United States Pharmacopeial Convention (usually also called the USP), a nonprofi ...
(USP) name gives the base drug name, followed by the radioisotope (as element symbol, space, mass number) with no parentheses, no hyphen, and no superscript, followed by the ligand (if any). The USP style is not the INN style, despite their being described as one and the same in some publications (e.g., '' AMA,'' whose style for radiopharmaceuticals matches the USP style). The United States Pharmacopeial Convention is a sponsor organization of the USAN Council, and the USAN for a given drug is often the same as the USP name.


See also

*
Radioactive tracer A radioactive tracer, radiotracer, or radioactive label is a synthetic derivative of a natural compound in which one or more atoms have been replaced by a radionuclide (a radioactive atom). By virtue of its radioactive decay, it can be used to ...
*
Nuclear medicine Nuclear medicine (nuclear radiology, nucleology), is a medical specialty involving the application of radioactivity, radioactive substances in the diagnosis and treatment of disease. Nuclear imaging is, in a sense, ''radiology done inside out'', ...


References


Further reading

* Notes for guidance on the clinical administration of radiopharmaceuticals and use of sealed radioactive sources. Administration of radioactive substances advisory committee. March 2006. Produced by the Health Protection Agency.
Malabsorption
In: The Merck Manual of Geriatrics, chapter 111.
Leukoscan summary of product characteristics
(Tc99m-Sulesomab). * Schwochau, Klaus. ''Technetium''. Wiley-VCH (2000).


External links


National Isotope Development Center
U.S. Government resources for isotopes - production, distribution, and information
Isotope Development & Production for Research and Applications (IDPRA)
U.S. Department of Energy program sponsoring isotope production and production research and development {{Nuclear technology Radiobiology Radiation therapy Medicinal chemistry Medicinal radiochemistry